ML324 (Synonyms: CID-44143209) |
| Catalog No.GC12557 |
ML324는 항바이러스 활성이 있는 강력한 JMJD2 데메틸라제 억제제입니다. ML324는 또한 4.9μM의 IC50으로 히스톤 데메틸라제 KDM4B에 대한 억제를 나타냅니다. ML324는 바이러스 IE 유전자 발현 억제를 통해 단순 헤르페스 바이러스(HSV) 및 인간 거대 세포 바이러스(hCMV) 감염 모두에 대해 강력한 항바이러스 활성을 가지고 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1222800-79-4
Sample solution is provided at 25 µL, 10mM.
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ML324 is a potent and cell-permeable JMJD2 demethylase inhibitor (IC50 = 920 nM). [1]
Jumonji-domain-containing proteins (JMJD) is the largest class of N ε -methyl lysine demethylase, an enzyme that demethylates the tri-methylated H3K9. JMJD takes part in gene transcription regulation. [1]
ML324 acted as an antiviral agent that effectively inhibited HSV and hCMV IE gene expression in HFF and MRC-5 cells, resulted in suppression of HSV plaques formation and inhibition of HSV infection spread. [1]
ML324 also blocked HSV-1 reactivation and inhibited the formation of HSV plaque in mouse ganglia explant model of latently infected mice. [1]
References:
1.Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR,
Dexheimer TS, Foley TL, King ON, Quinn A, Mott BT, Schofield CJ, Oppermann U,Jadhav A, Simeonov A, Kristie TM, Maloney DJ. Discovery of ML324, a JMJD2
demethylase inhibitor with demonstrated antiviral activity. 2012 Dec 17 [updated 2013 Sep 16]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
| Cell experiment [1]: | |
|
Cell lines |
HFF cells |
|
Preparation method |
The solubility of this compound in DMSO is > 17.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
5 ~ 50 μM |
|
Applications |
Compared with DMOG (IC50 = 0.75 mM), ML324 potently reduced IE gene expression, with an IC50 value of 10 μM. Besides, ML324 did not affect the expression of the cellular controls Sp1, S15 and TBP. In HFF cells infected with HSV-1, ML324 lowered viral yields in a dose-dependent manner (~ 4 ~ 5 logs at 25 μM) while 1.5 mM of DMOG was required to cause the same reduction. |
| Animal experiment [1]: | |
|
Animal models |
A mouse ganglia explant model of latently infected mice |
|
Dosage form |
50 μM; 48 hrs |
|
Applications |
In a mouse ganglia explant model of latently infected mice, ML324 significantly inhibited viral activity. At the concentration of 50 μM, ML324 reduced the viral yield by 4.5 logs for each ganglia. Immunofluorescent staining of explanted ganglia sections showed that ML324 inhibited viral reactivation events. However, the withdrawal of ML324 resulted in marked viral replication. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR, Dexheimer TS, Foley TL, King ON, Quinn A, Mott BT, Schofield CJ, Oppermann U,Jadhav A, Simeonov A, Kristie TM, Maloney DJ. Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity. 2012 Dec 17 [updated 2013 Sep 16]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. | |
| Cas No. | 1222800-79-4 | SDF | |
| Synonyms | CID-44143209 | ||
| Chemical Name | N-(3-(dimethylamino)propyl)-4-(8-hydroxyquinolin-6-yl)benzamide | ||
| Canonical SMILES | CN(CCCNC(C1=CC=C(C2=CC(O)=C3C(C=CC=N3)=C2)C=C1)=O)C | ||
| Formula | C21H23N3O2 | M.Wt | 349.43 |
| Solubility | ≥ 17.45mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8618 mL | 14.309 mL | 28.618 mL |
| 5 mM | 572.4 μL | 2.8618 mL | 5.7236 mL |
| 10 mM | 286.2 μL | 1.4309 mL | 2.8618 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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